1. Antibody-drug Conjugate/ADC Related Cell Cycle/DNA Damage
  2. ADC Payload Topoisomerase
  3. LD2-3

LD2-3 is a cytotoxic compound derived from Exatecan (HY-13631), designed to be conjugated with anti-FGFR2b or anti-CEA antibodies to form intact antibody-drug conjugate (ADC) molecules. LD2-3 exhibits a remarkable bystander killing effect: it not only effectively kills FGFR2b-positive tumor cells, but also eliminates surrounding FGFR2b-negative cells in co-culture and mixed tumor xenograft models, thereby inducing complete tumor regression. LD2-3 can be used for anti-tumor research in relevant fields such as gastric cancer and lung cancer.

For research use only. We do not sell to patients.

LD2-3

LD2-3 Chemical Structure

CAS No. : 3040077-52-6

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Description

LD2-3 is a cytotoxic compound derived from Exatecan (HY-13631), designed to be conjugated with anti-FGFR2b or anti-CEA antibodies to form intact antibody-drug conjugate (ADC) molecules. LD2-3 exhibits a remarkable bystander killing effect: it not only effectively kills FGFR2b-positive tumor cells, but also eliminates surrounding FGFR2b-negative cells in co-culture and mixed tumor xenograft models, thereby inducing complete tumor regression. LD2-3 can be used for anti-tumor research in relevant fields such as gastric cancer and lung cancer[1][2].

IC50 & Target

Topoisomerase I

 

In Vitro

BGA3457 (anti-FGFR2b antibody BGAh9179 conjugated to LD2-3) (34.75 ng/mL) exhibits potent bystander killing activity against FGFR2b-negative HuTu-80-NanoLuc cells cocultured with FGFR2b-positive SNU-16 cells, with an IC50 of 34.75 ng/mL and a maximum killing potency of 90.74%[1].
BGA3457 and BGA9823 (anti-FGFR2b antibodies conjugated to LD2-3) exhibit comparable internalization activity in SNU16, SNU601-h2b, H1048-h2b, and HSC-39 cell lines[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

LD2-3 (10 mg/kg; i.v.; single dose), as part of immunoconjugate FGFR2b-positive/negative gastric tumors in BALB/c nude mice[1].
LD2-3 (10 mg/kg; i.v.; single dose), as part of immunoconjugate BGA9823, induces complete regression of mixed FGFR2b-positive/negative gastric tumors in BALB/c nude mice[1].
LD2-3 (1-10 mg/kg; i.v.; single dose), as part of immunoconjugates BGA3457 and BGA9823, inhibits tumor growth in a FGFR2b-expressing gastric cancer xenograft model in BALB/c nude mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude (female, 6 to 8 weeks old)[1]
Dosage: 10 mg/kg (delivered as part of immunoconjugate BGA3457)
Administration: i.v.; single dose
Result: Induced complete tumor regression in both 2:1 and 5:1 HSC-39:SNU-5 co-inoculation models.
Molecular Weight

1244.28

Formula

C59H74FN11O18

CAS No.
SMILES

O=C(C=CC1=O)N1CC(NCCC(N[C@@H](CCC(NC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)CC(N)=O)=O)C(N[C@@H](C(C)C)C(N[C@@H](C)C(NCOCC(C)(C)C(N[C@@H]3C4=C5C(C(N6C5)=CC([C@](O)(C(OC7)=O)CC)=C7C6=O)=NC8=CC(F)=C(C)C(CC3)=C84)=O)=O)=O)=O)=O)=O

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Please store the product under the recommended conditions in the Certificate of Analysis.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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LD2-3
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HY-178238
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